高效液相色谱法对大鼠应用米非司酮的药物动力学研究  

Pharmacokinetics of Mifepristone following intragastric or Vaginal Administration in Rats by High Performance Liguid Chromatography

作　　者：刘昌官[1] 张国庆[1] 白秀梅[1] 顾林金[2] 

机构地区：[1]上海市计划生育科学研究所,上海200032 [2]上海医药工业研究院,上海200433

出　　处：《生殖与避孕》1997年第3期146-150,共5页Reproduction and Contraception

基　　金：国家计划生育委员会课题

摘　　要：用高效液相色谱法测定大鼠ig（灌胃）和阴道给药米非司酮（均为16mg／kg）后0.5、1、2、4、8、24、48h的血清浓度，根据各鼠血药浓度-时间数据拟会曲线，ig呈二室动力学模型，阴道给药呈一空动力学模型，其Tmax分别为2.43h、4.50h；Cmax分别为320．60μg／ml、129．64μg／ml；Ka分别为0．84／h、0．67／h；T1／2分别为（1）0．88h、0．98h；（2）1．65h、15．07h；Auc分别为5153．1μg·h／ml，3155．99μg·h／ml；K10分别为0．12／h，1．06／h。结果显示米非司酮ig血药浓度较阴道给药血药浓度为高。Mifepristone concentrations in serum were determiried by high performance liquid chro-matography (HPLC) at 0. 5, 1, 2,4, 8, 24 and 48 h after intragastric and vaginal administration inrats. According to concentration time course,the pharmacokinetic model of mifepristone in all ratsfollowed a pattern 0f two -compartment model after intragastric administrati0n and of one -c0m-partment after vaginal administration. The pharmacokinetic parameters were:Tm respectively 2.43 and 4. 5 h lCra respectively 320. 6 pg/ml and 129. 6 pg/ml1K' 0. 84/h and 0. 67/h $T,/,(1) O. 88h and 0. 98 h; (2) 1. 62 h and 15. 1 h;AUC 5153. 1 μg. h/ml and 315d. 99 μg· h/ml ；K10. 12/hand 1. 06/h. The concentration of serum mifepristone were higher by ig route adminstration thenby vaginal route;therefore, the early pregnancy termination efficacy was higher in former routeadministration.

关 键 词：高效液相色谱法 米非司酮 药物动力学 

分 类 号：R979.22[医药卫生—药品] R969.1[医药卫生—药学]